Quercetin loaded nanoemulsion-based gel for rheumatoid arthritis: In vivo and in vitro studies

[Display omitted] •Quercetin loaded nanoemulsion (QCT-NE) was developed and characterized.•QCT-NE was non-cytotoxic and inhibitory towards TNF-α production in cell line studies.•The QCT-NE gel Texture found to be suitable for the topical application after rheological and mechanical characterization....

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Veröffentlicht in:Biomedicine & pharmacotherapy 2019-04, Vol.112, p.108622, Article 108622
Hauptverfasser: Gokhale, Jayanti P., Mahajan, Hitendra S., Surana, Sanjay J.
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Sprache:eng
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Zusammenfassung:[Display omitted] •Quercetin loaded nanoemulsion (QCT-NE) was developed and characterized.•QCT-NE was non-cytotoxic and inhibitory towards TNF-α production in cell line studies.•The QCT-NE gel Texture found to be suitable for the topical application after rheological and mechanical characterization.•QCT-NE gel showed superior in vitro properties than free QCT gel.•In vivo antiarthritic studies revealed that QCT-NE gel is more efficient than free QCT gel. Current research reports the development, optimization and evaluation of Quercetin (QCT) loaded nanoemulsion (NE)-based gel for the effective rheumatoid arthritis (RA) management. The formulation of QCT- NE was developed using spontaneous emulsification techniques using the Box- Behnken experimental design. The cytotoxicity study and effect on TNF-α production were evaluated respectively on HIG-82 and RAW 264.7 cells. The study showed that QCT- NE has no toxic effect on synoviocytes and a strong inhibitory effect on LPS-induced TNF-α production. QCT- NE gel has confirmed adequate rheological behavior with a good texture profile and improved drug permeation compared to free QCT gel. In addition, the gel was found to be non-irritating and showed the inhibition of paw edema in rats induced by CFA over 24 h contrary to free QCT gel. In conclusion, the formulation of QCT- NE gel is an efficient topical treatment strategy for rheumatoid arthritis.
ISSN:0753-3322
1950-6007
DOI:10.1016/j.biopha.2019.108622